Spermicidal vaginal suppositories



United States Patent 0 SPERMICIDAL VAGINAL SUPPOSITORIES William C. Ward, Norwich, N. Y., assignor to The Norwich Pharmacal Company, Norwich, N. Y., a corporation of New York No Drawing. Application June 6, 1950, Serial No. 166,528

6 Claims. (Cl. 167-64) This invention relates to spermicidal vaginal suppositories.

The vaginal suppository which I have invented is particularly useful in the practice of feminine hygiene to secure inner cleanliness and in the elimination of objectionable odors. In the past, the practice of feminine hygiene has included the use of a vaginal douche consisting of an aqueous solution of a powerful antiseptic or the use of a vaginal suppository containing a small percentage of a powerful antiseptic followed by an aqueous vaginal douche. Deodorization of the vaginal tract as practiced in the past has consisted in the use of substances which possess odors designed to mask or cover up the less desirable odor whose elTect is sought to be overcome. Neither of these practices has been completely satisfactory: Many of the antiseptics which have been employed have a tendency to irritate the vaginal mucosa if used too frequently or it not sufiiciently diluted; and the odors of the substances which have been used to mask or cover up the less desirable odors in the vaginal tract are in themselves subject to objection.

I have discovered that a small percentage (about 0.2%) of a quaternary ammonium compound can be incorporated in a waxy vehicle or base comprising a non-ionic, surface-active, hydrophilic material which is solid at normal room temperatures but which melts rapidly at inner body temperature (37 C.) to provide a non-irritating suppository which is both antiseptic and deodorant and which also possesses valuable spermicidal activity. The quaternary ammonium compounds which I use as active antiseptic, deodorant and spermicidal agent in the practice of my invention are represented by the formula:

CH3 CH3 "ice nary ammonium compound at which this result is achieved is well below the toxic level of that material and at such concentration it is well tolerated by the vaginal mucosa and causes no irritation or other untoward reactions therein.

The vaginal suppositories embodying my invention are substantially odorless and it is evident that the deodorizing action thereof is due to the elimination rather than the masking of objectionable odors in the vaginal tract.

In order that my invention will be fully available to those skilled in the art, some formulations for the preparation of suppositories embodying my invention will be described briefly:

Example 1 Parts by weight A. Sorbitan monostearate polyoxyethylene derivative containing 4 oxyethylene units per mol 60.0 B. Sorbitan monolaurate polyoxyethylene derivative containing 20 oxyethylene units per mol 39.8 C. Hyarnine 10-X 0.2

A suppository is prepared from this formulation by heating and mixing ingredients A and B, which comprise the base, and ingredient C is dissolved in the molten mixture of ingredients A and B. The melted mass is then molded in the form of a suppository and allowed to cool and harden.

Example 2 Parts by weight A. Polyoxyethylene palmitate containing 20 oxyethylene units per mol 99.8 B. Hyamine 10-X 0.2

CH3 urn-c-cre-tF-Gocmomoamoral-0mg 01- E20 CH3 CH3 H3 in which X=H or CH3.

The two compounds which are represented by the above formula are, respectively: di-isobutyl cresoxy ethoxy ethyl dimethyl benzyl ammonium chloride, monohydrate; and di-isobutyl phenoxy ethoxy ethyl dimethyl benzyl ammonium chloride, monohydrate. Each of those compounds is at present marketed by Rohm &

'Haas Company, Washington Square, Philadelphia 5,

Pennsylvania. The former is marketed under the trade name Hyamine 10-X and the latter is marketed under the trade name Hyamine 1622. For purposes of brevity, those compounds will be referred to herein by those trade names.

The waxy base or vehicle which I prefer to use in the practice of my invention does not irritate the vaginal mucosa. It melts within a few minutes after it has been placed in the vagina to provide a liquid which, by virtue of its hydrophilic and surface-active character, emulsifies itself in the aqueous body fluids and rapidly coats the vaginal walls with a film which is rendered antiseptic, spermicidal and deodorizing by the quaternary ammonium compound, and which affords to the quaternary ammonium compound an optimum oppor tunity to function. The concentration of the quater- CHI Ingredients A, B and C, which comprise the base, are heated and mixed, and ingredient D is dissolved in the molten mixture. The melted mass is then molded in the form of a suppository and allowed to cool and harden.

In each of the above formulations, Hyamine 1622 may be substituted for Hyamine lO-X. Furthermore, the ingredients which are employed to provide the waxy base for the suppositories described in those specific embodiments of my invention may be replaced by other ingredients of like character. Changes in the suppository base may entail slight changes in the percentage of the Hyamine lO-X or Hyamine 1622 which is used. However, I prefer to maintain the proportion thereof at about 0.2% as I have found that vaginal suppositories containing such quaternary ammonium compounds at that concentration may be used as often as desired without causing irritation.

What I claim is:

1. A spermicidal, vaginal suppository comprising a base of non-ionic, hydrophilic, surface-active polyoxyethylene wax containing from about 4 to about 20 oxyethylene groups per mol which is solid at normal room temperatures and which melts rapidly at 37 C., and about 0.2% gt a qpaternary ammonium compound represented by the ormu a:

ignvghich X is a member of the group consisting of H and in dwgigt X is a member of the group consisting of H an 2. A spermicidal, vaginal suppository comprising a base 5. A spermicidal, vaginal suppository comprising 99.8

of non-ionic, hydrophilic, surface-active polyoxyethylene parts of polyoxyethylene palmitate containing 20 oxywax containing from about 4 to about 20 oxyethylene 5 ethylene units per mol, and 0.2 parts of a quaternary amgroups per mol which is solid at normal room temperamonium compound represented by the formula:

X CH: (3H3 (3H1 om-wB-om-c ocmcmo cinemas-031G 01- m0 CH3 (5H: (12H:

tures and which melts rapidly at 37 C., and about 0.2% of di-isobutyl cresoxy ethoxy ethyl dimethyl benzyl ammonium chloride, monohydrate.

3. A spermicidal, vaginal suppository comprising a base in which X is a member of the group consisting of H and of non-ionic hyclrophilig, sur flace-acltjive polyoxyettgylene wax containing rom a out to a out 20 oxye yene groups per mol which is solid at normal room tempera 6. A spermicidal, vaginal suppository comprising 50.0 Hes and which melts rapidly at 370 C. and about 02% 90 parts of cocoa butter, 42.0 parts of polyoxyethylene gm. of di-isobutyl phenoxy ethoxy ethyl dimethyl benzyl amcose distearate containing 6 oxyethylene units per mol, z g g gigf gzggfz gp y comprising-60 O 7.8 parts of polyoxyethylene sorbitol pentastearate conparts of sorbitan monostearate polyoxyethylene derivative tammg 6 oxyethylelle umts per and Parts of containing 4 oxyethylene units per mol, 39.8 parts of sor- 25 quaternary ammomum compound represented by the bitan monolaurate polyoxyethylene derivative containing formula:

x 0H; 0H; 0H; CHz-( J-CH:( 7 t -OCHzCHaOCHaCHr-Ik-CHaO Cl- H2O (13H: (3H3 4711a 20 oxyethylene units per mol, and 0.2 parts of a quaterin which X is a member of the group consisting of H and nary ammonium compound represented by the formula: CH3.

OH: CH: X GB: OHPACH:(IJ- D*O CHzOHaO CH2CH2J.\|ICH2C C1 H2O CH: CH: CH:

References Cited in the file of this patent UNITED STATES PATENTS 2,467,884 Elias Apr. 19, 1949 2,469,618 Ward et al. May 10, 1949 OTHER REFERENCES Lesser Drug and Cosmetic Industry, vol. 64, May 1949, pp. 631-634.

l7lgmd International Abstract of Surgery, July 1944, p.

Hyamines 1622 and 10- T Pamphlet from Rohm & Haas Co., Philadelphia. Copyright 1947, pp. 4, 12-13.

Baker, J. of Hygiene, vol. 31, April 1931, p. 212.

New and Nonoflicial Remedies, 1951, Philadelphia, J. P. Lippincott Co., pp. xxxi,

Swayne etc al., Proc. Soc. Exptl. Biol. and Med., vol. 80, No. 2, pp. 384 to 386. 

1. A SPERMICIDAL, VAGINAL SUPPOSITORY COMPRISING A BASE OF NON-IONIC, HYDROPHILIC, SURFACE-ACTIVE POLOXYETHYLENE WAX CONTAINING FROM ABOUT 4 TO ABOUT 20 OXYETHYLENE GROUPS PER MOL WHICH IS SOLID AT NORMAL ROOM TEMPERATURES AND WHICH MELTS RAPIDLY AT 37* C., AND ABOUT 0.2% OF A QUATERNARY AMMONIUM COMPOUND REPRESENTED BY THE FORMULA: 